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Assay Detail

CHEMBL4433813

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Transactivation of GAL4-tagged human PPARdelta LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Phenyldiazenyl Fibrate Analogues as PPAR α/γ/δ Pan-Agonists for the Amelioration of Metabolic Syndrome.
Giampietro L, Laghezza A, Cerchia C, Florio R, Recinella L, Capone F, Ammazzalorso A, Bruno I, De Filippis B, Fantacuzzi M, Ferrante C, Maccallini C, Tortorella P, Verginelli F, Brunetti L, Cama A, Amoroso R, Loiodice F, Lavecchia A.
ACS Med Chem Lett (2019) 10 : 545 -551
PubMed 30996794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 5.66 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153057 1 6.68
CHEMBL4533822 1 5.96
CHEMBL4461949 1 5.92
CHEMBL4592451 1 5.85
CHEMBL4445737 1 5.75
CHEMBL4444322 1 5.64
CHEMBL4449760 1 5.55
CHEMBL4557173 1 5.55
CHEMBL4471853 1 5.51
CHEMBL4453610 1 5.41
CHEMBL4580572 1 5.39
CHEMBL4461490 1 5.19
CHEMBL2204696 1 5.19
CHEMBL4438226 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153057 EC50 = 210.0 nM 6.68
CHEMBL4533822 EC50 = 1100.0 nM 5.96
CHEMBL4461949 EC50 = 1200.0 nM 5.92
CHEMBL4592451 EC50 = 1400.0 nM 5.85
CHEMBL4445737 EC50 = 1800.0 nM 5.75
CHEMBL4444322 EC50 = 2300.0 nM 5.64
CHEMBL4449760 EC50 = 2800.0 nM 5.55
CHEMBL4557173 EC50 = 2800.0 nM 5.55
CHEMBL4471853 EC50 = 3100.0 nM 5.51
CHEMBL4453610 EC50 = 3900.0 nM 5.41
CHEMBL4580572 EC50 = 4100.0 nM 5.39
CHEMBL4461490 EC50 = 6500.0 nM 5.19
CHEMBL2204696 EC50 = 6400.0 nM 5.19
CHEMBL4438226 EC50 - -